Antibactérien

Rosoxacin (Acrosoxacin) shows antibacterial activities against a broad spectrum of Gram-negative bacteria including Neisseria gonorrhoeae (MIC90 = 0.03mg/ml).

Elastase LasB-IN-1 (Compound 4b), a potent and selective inhibitor of elastase LasB, exhibits antibacterial activity and has been determined to possess an IC50

Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on

TP0480066 inhibits topoisomerase II, DNA gyrase (IC50=1.1nM), topo IV (IC50=62.89nM), effective against drug-resistant bacteria and N. gonorrhoeae.

Sulfisoxazole acetyl (Gantrisin) is an agent with antibacterial activity.

Zabofloxacin inhibits bacterial topoisomerases II/IV, effectively targeting gram-positive pathogens like S. aureus and S. pneumoniae.

CPFX2090, a cephalosporin antibacterial compound.

Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.

1,8-Dichloroanthraquinone, a derivative of anthraquinone, effectively inhibits sulfide production in sulfate-reducing bacteria [1].

Biotin-cholesterol, a biotinylated derivative of cholesterol, serves as a precursor in the manufacturing of biotin-conjugated liposomes and micelles, which are utilized in drug delivery systems [1].

Compound 5b, an antibacterial, effectively targets MRSA and disrupts bacterial membranes and PG synthesis.

4-Aminosalicylic acid hemicalcium, an orally active antibiotic, shows potential in tuberculosis research [1].

Quorum Sensing-IN-2 (compound 23e) is a quorum sensing inhibitor that curtails bacterial pathogenicity without impeding growth.

Tuberculosis Inhibitor 12, an oxadiazole derivative, effectively inhibits Mycobacterium tuberculosis, demonstrating inhibition rates of 82% and 78% at a

β-L-Gulopyranosyl-caldarchaetidyl-glycerol is the principal polar lipid in the archaeon T. acidophilum. Its cellular levels in T. acidophilum HO-62 show a positive correlation with culture pH and a negative correlation with temperature. This compound also serves as a standard for polar lipid quantification from T. acidophilum HO-62. [Matreya, LLC. Catalog No. 1303]

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.

Levofuraltadone is an antiprotozoal and antibacterial agent.

Dihydropleuromutilin, a semisynthetic antibiotic derived from pleuromutilin, exhibits antimicrobial efficacy against S. aureus, M. hominis, M. gallisepticum, and M. hyorhinis, with minimum inhibitory concentrations (MICs) of 0.5, 0.3, 0.3, and 2 µg/ml, respectively.

DCAP, a broad-spectrum antibiotic, disrupts the membranes of both Gram-positive and Gram-negative bacteria. Additionally, it inhibits late-stage autophagy by blocking autophagolysosome maturation and interrupting autophagic flux [1].

(+)-Thienamycin, a powerful broad-spectrum antibacterial and β-lactamase inhibitor, is isolated from Streptomyces cattleya [1].

Antibiofilm agent-9 (Compound 4), a derivative of pyrrolnitrin, exhibits antimicrobial activity. It inhibits Bacillus anthracis with a Minimum Inhibitory Concentration (MIC) of 0.031 μg/mL. The compound demonstrates significant antibiofilm activity, achieving an inhibition rate of 84% after 24 hours at a concentration of 8.0 μg/mL. Additionally, Antibiofilm agent-9 shows favorable pharmacokinetic properties in mouse models.

Du011 is a biogenesis inhibitor of the E.

Netropsin dihydrochloride, a small MGB, blocks topoisomerase I/II, hindering cleavable complex stabilization.

IpOHA is a potent inhibitor of plant KARI and functions as an antimycobacterial agent, demonstrating a K_i value of 97.7 nM against Mycobacterium tuberculosis (

TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.

Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].

β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor that can be used for researching

Valnemulin, a broad-spectrum pleuromutilin antibiotic, targets peptidyl transferase within the 50S ribosomal subunit, effectively used in veterinary medicine to address swine diseases such as B. hyodysenteriae and M. hyopneumoniae.

Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and

Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]

MsbA-IN-6: potent antibiotic, hinders MsbA in gram-negative bacteria, kills E. coli, effective on drug-resistant strains.

DHFR-IN-10 (compound 4c) is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an inhibition concentration half-maximum (IC50) of 4.21 μM against

Ianthelliformisamine B TFA, an antibiotic enhancer, is used to against resistant Gram-negative bacteria.

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

Δ2-transEicosenoic acid, an α,β-unsaturated fatty acid, emerges as a by-product during the synthesis of Δ2-ciseicosenoic acid, which along with its salts, shows promise in diabetes treatment and lipid metabolism enhancement. Additionally, the compound 2-octadecenoic acid is recognized for its ability to enhance liver function and reduce blood sugar levels in streptozocin-induced diabetic rats.

Despropylene gatifloxacin, a metabolite of AM-1155, exhibits potent antibacterial activity and has favorable pharmacokinetics [1].

DuP-721: broad-spectrum, oral antibiotic targeting various bacteria, including M. tuberculosis.

NSC309401 is an E. coli dihydrofolate reductase inhibitor with an IC50 value of 189 nM and a dissociation constant (Kd) of 14.57 nM [1].

Flurofamide is an effective bacterial urease inhibitor and has potential in the treatment of infected urinary calculi.

Sudoterb free base (Sudoterb) , also known as LL3858, is an anti-tubercular drug candidate.

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Antibiofilm Agent-1, as detailed in WO2017011725A1 (compound 17) [1], serves as an antibacterial agent effective against Gram-positive pathogens.

SCH-538415: Microbial acyl carrier protein synthase inhibitor, IC50 4.19µM; anti-Staphylococcus aureus.

NSC309401 is an E. coli dihydrofolate reductase inhibitor, displaying potency with an IC50 value of 189 nM and a dissociation constant (KD) of 14.57 nM [1].

Methyl 2-amino-5-bromobenzoate (Methyl 5-Bromoanthranilate) is an HCV NS5b RNA polymerase inhibitor with antimicrobial activity.

Mansonone F is a topoisomerase II inhibitor with cytotoxic and topo inhibitory potencies.

Isotianil is a plant defense inducer that activates typical plant defense responses without direct antimicrobial effects, serving as a plant protection agent

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

LY 173013 is a bicyclic pyrazolidinone, it has antibacterial properties.

LS-BF1: Stable, low-toxic antimicrobial peptide targeting ESKAPE pathogens via cell membrane disruption, effective in mouse infection model.

Avarofloxacin (JNJ-Q2) is a fluoroquinolone for treating bacterial skin infections and pneumonia.

4-Nitrophenyl palmitate serves as a colorimetric substrate for lipase and esterase, enabling the quantification of enzyme activity through the release and colorimetric detection of 4-nitrophenol at 410 nm following enzymatic hydrolysis. This compound facilitates the characterization of enzyme activity across diverse bacterial and mammalian sources, including Burkholderia and porcine pancreatic lipases.

A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.

T145 halts key bacteria growth at sub μg/ml, deters resistance, and may enhance drug lifespan.

A7132 is an antibacterial agent and possesses broad and potent antibacterial activity.

Contezolid (MRX-I) is an antibiotic with bactericidal activity and can be used to study tuberculosis.

Salicyl-AMS is an inhibitor of mycobacterium auxin biosynthesis that inhibits the growth of mycobacterium in the presence of iron deficiency in vitro.

Supercinnamaldehyde is a potent activator of transient receptor potential ankyrin 1 (TRPA1), exhibiting an EC50 of 0.8 μM, and induces activation of TRPA1 ion

DHFS-IN-1 (Compound 3) is an inhibitor of dihydrofolate synthetase (DHFS) with an IC50 of 2.6 μM. It is applicable for research into infectious diseases related to bacterial folate synthesis.

D-CS319 is a potent inhibitor of metal-𝛽-lactamases (MBLs), exhibiting IC50 values of 2.0 μM for IMP-1 and 3.0 μM for IMP-78. RPX 7546 possesses antibacterial activity.

Novel anti-TB agent 62 is a redox compound with bactericidal activity against active and dormant bacteria.

Atramycin A is an anthraquinone antibiotic with antitumor properties.

Compound 6q, a trifluoromethylpyridine oxadiazole, targets Xanthomonas oryzae with EC50 of 7.2 μg/mL.

MsbA-IN-3 is a potent and highly selective MsbA inhibitor (IC50: 2 nM). MsbA-IN-3 inhibits Escherichia coli activity (MIC: 35 μM).

Compound 11i: potent, non-toxic anti-tuberculosis biphenyl analogue.

PptT-IN-3 (5p), an inhibitor of PptT in Mycobacterium tuberculosis, IC50=3.5μM, is key for TB research.

RhlR antagonist 1: IC50 of 26 μM, selective for RhlR, inhibits P. aeruginosa biofilm and virulence factors.

Meclocycline: a tetracycline antibiotic, inhibits LDH, reduces cell toxicity from mutant huntingtin, doesn't change protein levels in PC12 cells.

Antifungal agent 38, a heterocyclic disulfide, shrinks hyphae and damages cell membranes, causing leakage.

Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent with low cytoxicity for MCF-7, A549 cells [1].

PCTR1, derived from DHA, hastens inflammation resolution and boosts macrophage function, reducing PGE2, PGD2, and TXB2 in mice.

MtTMPK-IN-7 inhibits MtbTMPK (IC50: 47 μM), active against M. brevis (MIC: 2.3-4.7 μM), useful for tuberculosis research.

Cefoxazole is a β-lactam antibiotic featuring an isoxazole structure, known for its antibacterial activity. It can be utilized in the study of infectious diseases.

Anticaries agent-1 (Compound 21b) is utilized as an anticaries agent. It effectively inhibits biofilm formation with an IC50 of 77 μM and restricts the growth of S. mutans.

MtTMPK-IN-3 inhibits Mycobacterium tuberculosis kinase with IC50 0.12μM, MIC 12.5μM on Mtb, cytotoxic EC50 12.5μM on MRC-5 cells.

MraY-IN-3 (12a) is a potent inhibitor of the bacterial translocase MraY (IC50: 140 μM). 46 μg/ml).

MtMetAP1-IN-1 is an inhibitor of methionine aminopeptidase 1 ( MetAP1 ). MtMetAP1-IN-1 shows antimycobacterial activity.

Compound 3d: antitubercular, MIC 0.007 μg/mL vs MTB H37Rv, 1.851 μg/mL vs MDR-MTB 16833, metabolically unstable.

MsbA-IN-5 (compound 40) is a potent and highly selective inhibitor of MsbA (IC50: 2 nM). MsbA-IN-5 can be used in Gram-negative studies.

Gln-AMS (TFA) is a type Ia amido-tRNA synthetase (AARS) inhibitor with a Ki value of 1.32 μM for glutaminyl-tRNA synthetase.

Antibacterialagent 279 (compound A12) is an effective antibacterial agent. It inhibits the SOS response of Pseudomonas aeruginosa.

BM635 hydrochloride, an MmpL3 inhibitor, strongly blocks Divergent bacteriophage H37Rv (MIC50: 0.08 μM), with doubled in vivo potency.

Antibiofilm agent-14 (compound 11) functions as an antibiofilm agent. It exhibits antifungal activity against C.albicans SC5314, with a minimum inhibitory concentration (MIC) of 50 μM.

BM635 mesylate inhibits MmpL3; kills Divergent bacterium with 0.6 µM MIC50; boosts bioavailability.

DC-159a, an 8-methoxy fluoroquinolone, possesses broad-spectrum antibacterial activity, with a particular efficacy against Gram-positive pathogens. The MIC90 values for DC-159a are 0.5 μg/mL against Streptococcus anginosus group, 4 μg/mL against Clostridium difficile, and 2 μg/mL against Bacteroides fragilis.

DL-2-Aminopimelic Acid acts as a weak agonist for glutamate receptors and also reduces the sensitivity of leech glutamate receptors to glutamate.

4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.

MetRS-IN-1 (Compound 27) is an inhibitor of E. coli methionyl-tRNA synthetase (MetRS) with an IC50 value of 237 nM [1].

Rf470 (Rotor NO.4) TFA is an FMR-probe-D-lysine conjugate (Max Ex: 470 nM; Max Em: 640 nM) that can be covalently integrated into bacterial peptidoglycan. In its free state, Rf470 TFA exhibits weak fluorescence, which significantly increases upon integration into peptidoglycan by transpeptidase catalysis. This fluorescence change allows Rf470 TFA to be used for real-time monitoring of peptidoglycan biosynthesis, detecting transpeptidase activity, and screening antibiotics.

Anti bacterial agent 236 (Compound 4l), an orally effective inhibitor of DNA gyrase and topoisomerase IV (with IC50 values of 3.2 and 300 nM in Staphylococcus aureus, respectively), exhibits broad-spectrum antibacterial activity. It also demonstrates favorable pharmacokinetic properties in mice.

Cetefloxacin (E 4868) is a broad-spectrum antibacterial antibiotic with a minimum inhibitory concentration (MIC) ranging from 0.007 to 8 µg/ml. In mice, cetefloxacin demonstrates favorable pharmacokinetic properties and provides protection against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.

NBTIs-IN-5 inhibits Mycobacterium abscessus DNA with IC50 1.5μM, halts growth at MIC90 0.4μM.

Compound 8b inhibits VEGFR-2/DHFR, combats various bacteria, and fights cancer cells.

MraY-IN-2 (compound 6) is an effective inhibitor of bacterial transposase MraY (IC50=4.5 μ M), and can be used for antibacterial research.

G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter protein. G092 has potential for antibacterial drug research.